Alendronate Sodium (Fosamax)

Introduction

Alendronate Sodium, which is marketed as Fosamax, is known as a bisphoshonate medication utilized for treating osteogenesis imperfecta, osteoporosis, and a number of other bone diseases. It belongs to Bisphosphonate medication group, which stands for chemically solid derivatives of anorganic pyrophosphate (Sun, Liu, Sun, Lu & Ning, 2012). Due to their similarity with the main bone element (hydroxyapatite), they are integrated into locations of active osteoclast-conciliated bone reabsorbing on the bone exterior elevating bone density locally, where they might effect osteoclast activity (Sun et al., 2012). Bisphosphonates appear to be highly hydrophilic and are badly removed from the gastrointestinal tract. When they are occluded, skeletal retention is believed to repulse host facets and bisphosphonate effectiveness for bone matrix (Kennel & Drake, 2009). These facts demonstrate that bisphosphonates are broadly administered and greatly efficacious in restricting the bone detriment, which appears in numerous bone disorders (Sun et al., 2012). Regardless of the fact that they are typically well-tolerated, possible adverse impacts might restrict bisphosphonate usage in a number of patients. Optimal utilization of bisphosphonates for osteoporosis requires appropriate calcium and vitamin D consumption prior and during the therapy (Kennel & Drake, 2009). 

Generic and Brand Name

The generic name appears as Alendronate (a LEN dro nate), while Alendronate Sodium’s brand names incorporate Fosamax and Binosto (Gould & Dyer, 2011).

Pharmacokinetics

Pharmacokinetics incorporates absorption, distribution, metabolism, and elimination. This drug’s absorption demonstrates that Alendronate Sodium’s oral bioavailability accounts for 0.64 percent (for females) and 0.59 percent (for males) (Gould & Dyer, 2011). It is also important to mention that food significantly reduces the drug’s bioavailability. Review of Alendronate Sodium’s distribution demonstrates that it is first distributed to soft tissues and then – to bones. The volume of distribution (Vd) typically stands for minimum 28 L (units of volume), which appears to be exclusive of bone, while approximately 78 percent belongs to protein connection (Gould & Dyer, 2011). The analysis of metabolism demonstrates that the drug is not metabolized. Finally, the elimination review reveals that approximately 50 percent of the drug is excreted in urine within 72 hours (Gould & Dyer, 2011). The biological half-life (t ½) stands for more than 10 years (Gould & Dyer, 2011). Nonetheless, the elimination might be lowered. Moreover, no dosage regulation is indispensable in those patients who have mild to moderate nephritic function impairment. However, it is important to mention that Alendronate Sodium is not recommended for those patients who appear to have severe nephritic function aggravation (Ccr has to be lower than 35 mL/min).

Pharmacodynamics

The pharmacodynamics review of Alendronate Sodium demonstrates that it is a second-generation bisphosphonate at the same time being the initial member of a drug group, which consolidates bones (Gould & Dyer, 2011). Thus, Alendronate is utilized to lower the hypercalcemia in tumor-enforced bone disease in order to medicate corticosteroid-generated Paget’s disease and osteoporosis and impede osteoporosis in postmenopausal females. In fact, the inhibition of osteoclastic bone resorption with no impact on bone formation, specifically at locations of active resorption, appears to be highly characteristical of Alendronate Sodium (Ochiuz et al., 2016). This leads to the fact that qualitatively ordinary bones are formulated. The facts demonstrate that in pharmacology Alendronate appears to be approximately 700 times more efficient as compared to etidronate. Also, it is 100 times more influential when compared to clodronate, and 10 times more efficacious than pamidronate in vivo even despite the fact that its PK (Pharmacokinetics) is analogous to other bisphosphonates (Gould & Dyer, 2011).

Indications and Usage

Alendronate Sodium is used to prevent and medicate osteoporosis in postmenopausal females, elevate bone mass in males, treat glucocorticoid-enforced osteoporosis in both males and females, and relieve symptoms of Paget bone disease (Ochiuz et al., 2016).

Contraindications

The facts demonstrate that Alendronate Sodium tablets appear to be contraindicated for patients with a number of conditions including malfunctions of the esophagus, which procrastinate esophageal emptying such as stricture or achalasia (Gould & Dyer, 2011). The second contraindicated encompasses the incapability to stand or sit upright for minimum 30 minutes (Gould & Dyer, 2011). Also, people with Hypocalcemia should not use this drug. The final condition that does not allow using Alendronate Sodium is hypersensitivity to any constituent of this product (Gould & Dyer, 2011). Hypersensitivity reactions typically incorporate angioedema and urticaria (Gould & Dyer, 2011).

Side Effects

The facts demonstrate that the medication involving Alendronate Sodium tablets might lead to such side effects as stomach ache, diarrhea, constipation, or nausea. In case the above-mentioned effects remain or aggravate, it is highly important to immediately address a doctor or pharmacist (Ochiuz et al., 2016). While analyzing the side effects, it is crucial to understand that the medication has been prescribed because the benefit is higher than the hazard of side effects. Numerous patients utilizing this medication do not have solid side effects. More severe side effects typically incorporate jaw ache, elevation or severe bone/joint/muscle ache, novel or unprecedented hip/thigh/groin ache, swelling of joints/hands/feet/ankles, tarry/black stools, or vomiting, which resembles coffee grounds (Ochiuz et al., 2016).

This medication might seldom provoke solid or highly demure allergic reactions, ulcers and irritation of the esophagus. However, if the patient notices above-mentioned side effects together with rash, itching/swelling (especially of the face/tongue/throat), dizziness, and troubled breathing, it is important to stop taking Alendronate Sodium (Ochiuz et al., 2016).

Normally, the announced side effects of Alendronate incorporate lowered level of serum calcium and reduced level of serum phosphate. Some other side effects encompass arthralgia, myalgia, and ostealgia. Side effects can be subdivided into several categories depending on the organism system impact. The first category concerns gastrointestinal tract leading to ulceration of the esophagus (Ochiuz et al., 2016). These side effects might even require hospitalization and intensive treatment. Another side effect concerns esophageal cancer. In fact, a meta-analysis vividly demonstrates that bisphosphonate medication is closely connected to the excess hazard of esophageal cancer (Ochiuz et al., 2016). The second category regards general side effects, which incorporate infrequent cases of skin rash and eye issues (uveitis or scleritis). The laboratory tests demonstrate that calcium and phosphate values might be lowered (Ochiuz et al., 2016). Nevertheless, these tests vividly repulse the drug action, which is harmless. Thirdly, it is important to state that in case when any type of dental work is performed during the drug medication, it might lead to osteonecrosis of the jaw, which stands for the deterioration of the temporomandibular joint. Regardless of the fact that the above-mentioned side effect is untypical, it appears originally in patients, which are administered to intravenous biphosphonates medication (Ochiuz et al., 2016). The final category stands for bones. The facts demonstrate that Alendronate has been connected in long-range users with the evolvement of low-influence femoral fractures. In addition, numerous researches demonstrate that users of Alendronate Sodium appear to have an elevation in the quantities of osteoclasts and develop more multinucleated osteoclasts (Ochiuz et al., 2016). Furthermore, the facts demonstrate that Fosamax has been connected to a rare kind of leg fracture, which cuts straight across the upper thighbone after a minor or no trauma (known as subtrochanteric fractures) (Ochiuz et al., 2016).

Adverse Effects

Medications involving Alendronate Sodium might lead to adverse reactions. Firstly, they might concern the central nervous system causing headaches or malaise (Gould & Dyer, 2011). Secondly, they might lead to dermatologic complicacies encompassing pruritus, rash (might be combined with photosensitivity), solid skin reactions covering Stevens-Johnson syndrome and toxic epidermal necrolysis. Thirdly, adverse effects might affect EENT (eye, ear, nose, and throat) leading to episcleritis, scleritis or uveitis (Gould & Dyer, 2011). Fourthly, the drug might affect gastroenterological system triggering abdominal ache, acid regurgitation, flatulence, esophageal ulcer, gastric ulcer, gastritis, duodenal ulcer, esophagitis, esophageal erosion, esophageal stricture or perforation (Ochiuz et al., 2016). Fifthly, the medication might lead to hypersensitivity, encompassing urticaria and angioedema (Gould & Dyer, 2011). Finally, the drug might negatively influence musculoskeletal system resulting in muscular skeletal pain, muscle cramps, or transient myalgia (Ochiuz et al., 2016).

Patient Variables

The analysis of geriatric variable demonstrates that bioavailability and disposition (meaning urinary excretion) appeared to be analogous with regard to younger and elderly patients. It is also important to mention that elderly patients do not require any dosage adjustments. The review of pediatric variable reveals that the oral bioavailability in children appeared to be analogous to the one, which is observed in adults (Ochiuz et al., 2016). Nevertheless, Alendronate Sodium cannot be suggested for usage in children. The analysis of pregnancy variable vividly shows that it might have teratogenic impacts making the case of category C pregnancy (Ochiuz et al., 2016). It is important to mention that no researches have been conducted in regard to pregnant females. Thus, Alendronate Sodium should be utilized during pregnancy merely in the case when the possible advantage exculpates the feasible hazard to the mother and fetus despite the fact that there are no data on fetal hazard in humans (Gould & Dyer, 2011). Nevertheless, there is a theoretical hazard of fetal detriment, predominantly skeletal in case when a woman becomes pregnant after finalizing a course of bisphosphonate therapy (Ochiuz et al., 2016). Finally, the analysis of lactation variable shows that it is actually unknown whether Alendronate gets into the human milk (Gould & Dyer, 2011). Due to the fact that numerous drugs are actually excreted in human milk, caution should be voided when the analyzed medicine is dispensed to breast-feeding females (Gould & Dyer, 2011).

Off-Label Uses

Off-label usages, which stand for the non-FDA approved utilizations, typically incorporate vitamin D overdose and osteoporosis provoked by spinal trauma (Ochiuz et al., 2016). Despite the fact that the drug is utilized off-label for some children suffering from metabolic bone disease, researches of Alendronate have actually failed to establish the effectiveness or security for this age group.